P
US4028319AExpiredUtilityPatentIndex 70

2 and 3-substituted enkephalins

Assignee: SEARLE & COPriority: May 7, 1976Filed: May 7, 1976Granted: Jun 7, 1977
Est. expiryMay 7, 1996(expired)· nominal 20-yr term from priority
Inventors:JONES JR DAVID ASCHLATTER JAMES MMIKULEC RICHARD AREUTER JUDITH AMAZUR ROBERT H
A61P 25/00A61P 25/04A61P 25/30A61P 1/12A61K 38/00C07K 5/06026C07K 14/702
70
PatentIndex Score
12
Cited by
3
References
23
Claims

Abstract

Analogs of enkephalin having agonist activity at opiate receptors are disclosed herein. These analogs are useful as analgesics, non-addicting narcotic antagonists and anti-diarrheal agents.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A compound of the formula   H--Tyr--W--Phe--Y--OH                                      (I)     wherein Y is Leu or Met; W is selected from the group consisting of   --Aib--Gly--,   --Ala--Gly--,   --Sar--Gly--,   --Gly--Aib--,   --Gly--Ala--,   --Gly--Sar--, ##STR9## and the stereochemical configuration of each of the optically active amino acid residues is D, L or DL.   
     
     
       2. A compound according to claim 1 of the formula   H--Tyr--W--Phe--Y--OH                                      (II)     wherein Y is Leu or Met; W is selected from the group consisting of   --Aib--Gly--,   --Ala--Gly--,   --Sar--Gly--,   --Gly--Aib--,   --Gly--Ala--,   --Gly--Sar--, ##STR10## and the stereochemical configuration of each of the optically active amino acid residues is L.   
     
     
       3. A compound according to claim 1 of the formula   H--Tyr--Z--Gly--Phe--Y--OH     wherein Z is Aib, Ala or Sar; Y is Leu or Met; and the stereochemical configuration of each of the optically active amino acid residues is L.   
     
     
       4. A compound according to claim 1 of the formula   H--Tyr--Gly--Z--Phe--Y--OH     wherein Z is Aib, Ala or Sar; Y is Leu or Met; and the stereochemical configuration of each of the optically active amino acid residues is L.   
     
     
       5. A compound according to claim 1 of the formula   H--Tyr--W--Phe--Y--OH     wherein Y is Leu or Met; W is ##STR11## and the stereochemical configuration of each of the optically active amino acid residues is L.   
     
     
       6. The compound according to claim 1 which is L-tyrosyl-L-alanylglycyl-L-phenylalanyl-L-methionine. 
     
     
       7. The compound according to claim 1 which is L-tyrosyl-L-alanylglycyl-L-phenylalanyl-L-leucine. 
     
     
       8. The compound according to claim 1 which is L-tyrosylsarcosylglycyl-L-phenylalanyl-L-methionine. 
     
     
       9. The compound according to claim 1 which is L-tyrosylsarcosylglycyl-L-phenylalanyl-L-leucine. 
     
     
       10. The compound according to claim 1 which is L-tyrosylglycyl-L-alanyl-L-phenylalanyl-L-methionine. 
     
     
       11. The compound according to claim 1 which is L-tyrosylglycyl-L-alanyl-L-phenylalanyl-L-leucine. 
     
     
       12. The compound according to claim 1 which is L-tyrosylglycylsarcosyl-L-phenylalanyl-L-methionine. 
     
     
       13. The compound according to claim 1 which is L-tyrosylglycylsarcosyl-L-phenylalanyl-L-leucine. 
     
     
       14. The compound according to claim 1 which is L-tyrosyl-5-aminopentanoyl-L-phenylalanyl-L-methionine. 
     
     
       15. The compound according to claim 1 which is L-tyrosyl-5-aminopentanoyl-L-phenylalanyl-L-leucine. 
     
     
       16. The compound according to claim 1 which is L-tyrosyl-p-aminobenzoyl-L-phenylalanyl-L-methionine. 
     
     
       17. The compound according to claim 1 which is L-tyrosyl-p-aminobenzoyl-L-phenylalanyl-L-leucine. 
     
     
       18. The compound according to claim 1 which is L-tyrosyl-α-aminoisobutyrylglycyl-L-phenylalanyl-L-methionine. 
     
     
       19. The compound according to claim 1 which is L-tyrosyl-α-aminoisobutyrylglycyl-L-phenylalanyl-L-leucine. 
     
     
       20. The compound according to claim 1 which is L-tyrosylglycyl-α-aminoisobutyryl-L-phenylalanyl-L-methionine. 
     
     
       21. The compound according to claim 1 which is L-tyrosylglycyl-α-aminoisobutyryl-L-phenylalanyl-L-leucine. 
     
     
       22. The compound according to claim 1 which is D-tyrosylglycyl-D-alanyl-D-phenylalanyl-D-leucine. 
     
     
       23. The compound according to claim 1 which is DL-tyrosylglycyl-DL-alanyl-DL-phenylalanyl-DL-leucine.

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